JP3898220B2 - レボブピバカインおよびその類似体の製造に使用するラセミ化と不斉変換法 - Google Patents

レボブピバカインおよびその類似体の製造に使用するラセミ化と不斉変換法 Download PDF

Info

Publication number
JP3898220B2
JP3898220B2 JP51069496A JP51069496A JP3898220B2 JP 3898220 B2 JP3898220 B2 JP 3898220B2 JP 51069496 A JP51069496 A JP 51069496A JP 51069496 A JP51069496 A JP 51069496A JP 3898220 B2 JP3898220 B2 JP 3898220B2
Authority
JP
Japan
Prior art keywords
acid
racemization
compound
pct
asymmetric transformation
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
JP51069496A
Other languages
English (en)
Japanese (ja)
Other versions
JPH10505855A (ja
Inventor
ダイヤー,ウルリッヒ・コンラッド
ロック,クリストファー・ジェイムズ
ウッズ,マーティン
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Darwin Discovery Ltd
Original Assignee
Darwin Discovery Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB9504927.6A external-priority patent/GB9504927D0/en
Application filed by Darwin Discovery Ltd filed Critical Darwin Discovery Ltd
Publication of JPH10505855A publication Critical patent/JPH10505855A/ja
Application granted granted Critical
Publication of JP3898220B2 publication Critical patent/JP3898220B2/ja
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B53/00Asymmetric syntheses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B55/00Racemisation; Complete or partial inversion

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
  • Saccharide Compounds (AREA)
  • Measurement Of Radiation (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
JP51069496A 1994-09-23 1995-09-22 レボブピバカインおよびその類似体の製造に使用するラセミ化と不斉変換法 Expired - Lifetime JP3898220B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP94306962 1994-09-23
GB94306962.5 1995-03-10
GBGB9504927.6A GB9504927D0 (en) 1995-03-10 1995-03-10 Racemisation and asymmetric transformation
GB9504927.6 1995-03-10
PCT/GB1995/002247 WO1996009290A1 (en) 1994-09-23 1995-09-22 Racemisation and asymmetric transformation processes used in the manufacture of levobupivacaine and analogues thereof

Publications (2)

Publication Number Publication Date
JPH10505855A JPH10505855A (ja) 1998-06-09
JP3898220B2 true JP3898220B2 (ja) 2007-03-28

Family

ID=26137306

Family Applications (1)

Application Number Title Priority Date Filing Date
JP51069496A Expired - Lifetime JP3898220B2 (ja) 1994-09-23 1995-09-22 レボブピバカインおよびその類似体の製造に使用するラセミ化と不斉変換法

Country Status (18)

Country Link
US (1) US5786484A (pt)
EP (1) EP0782569B1 (pt)
JP (1) JP3898220B2 (pt)
KR (1) KR100393133B1 (pt)
CN (1) CN1104416C (pt)
AT (1) ATE214695T1 (pt)
AU (1) AU695479B2 (pt)
CA (1) CA2200490C (pt)
DE (1) DE69525950T2 (pt)
DK (1) DK0782569T3 (pt)
ES (1) ES2173194T3 (pt)
FI (1) FI117436B (pt)
HU (1) HU216291B (pt)
MX (1) MX9702210A (pt)
NO (1) NO308074B1 (pt)
PL (1) PL183204B1 (pt)
PT (1) PT782569E (pt)
WO (1) WO1996009290A1 (pt)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6384227B2 (en) 1995-01-18 2002-05-07 Darwin Discovery Ltd. Racemisation process for use in the manufacture of levobupivacaine and related piperidinecarboxanilide anaesthetic agents
JP2000256359A (ja) * 1999-03-11 2000-09-19 Japan Science & Technology Corp 面性キラリティーを有する分子群の高選択的不斉変換法
US6288280B1 (en) * 1999-07-09 2001-09-11 Hoffmann-La Roche Inc. Racemization of atropisomeric bis(phosphine oxide) compounds
BR0002246A (pt) 2000-04-06 2003-04-15 Cristalia Prod Quimicos Farm Processo de obtenção dos enantiÈmeros da bupivacaìna racêmica, processo de obtenção de composições farmacêuticas a base de levobupivacaìna: composições farmacêuticas a base de levobupivacaìna formuladas nas formas básicas ou sais farmaceuticamente aceitáveis e utilização das composições farmacêuticas a base de levobupivacaìna formuladas nas formas básicas ou sais farmaceuticamente aceitáveis
US6962998B2 (en) 2000-06-14 2005-11-08 Toray Industries, Inc. Processes for producing racemic piperidine derivative and for producing optically active piperidine derivative
DE10029851A1 (de) * 2000-06-16 2001-12-20 Boehringer Ingelheim Pharma Enantiomerentrennung von Piperidon-Derivaten unter gleichzeitiger in situ Racemisierung des unerwünschten Enantiomers
US6495694B2 (en) 2000-06-16 2002-12-17 Boehringer Ingelheim Pharma Kg Efficient separation of enantiomers of piperidone derivatives by precipitation of the desired eantiomer during in situ racemization of the unwanted enantiomer
BRPI0104491B8 (pt) * 2001-10-10 2021-05-25 Cristalia Produtos Quim Farmaceuticos Ltda n-(2,6-dimetilfenil)-1-propil-2-piperidinocarboxamida; processo de obtenção dos enantiômeros; mistura não racêmica dos anantiômeros e seu processo de obtenção e composição farmacêutica.
US20040001889A1 (en) 2002-06-25 2004-01-01 Guohua Chen Short duration depot formulations
EP2218448B1 (en) 2002-12-13 2015-09-23 Durect Corporation Oral drug delivery system comprising high viscosity liquid carrier materials
CA2581287C (en) * 2004-09-17 2015-08-25 Durect Corporation Sustained local anesthetic composition containing bupivacaine and saib
US20070027105A1 (en) 2005-07-26 2007-02-01 Alza Corporation Peroxide removal from drug delivery vehicle
AU2007325918B2 (en) 2006-11-03 2013-10-17 Durect Corporation Transdermal delivery systems comprising bupivacaine
JP2011506319A (ja) 2007-12-06 2011-03-03 デュレクト コーポレーション 疼痛、関節炎症状、または慢性疾患に伴う炎症の治療に有用な方法
US20100260844A1 (en) 2008-11-03 2010-10-14 Scicinski Jan J Oral pharmaceutical dosage forms
CN102093284B (zh) * 2010-12-29 2013-05-08 宜昌人福药业有限责任公司 富集哌啶-2-甲酰苯胺类旋光化合物的方法
AU2014233453A1 (en) 2013-03-15 2015-10-01 Durect Corporation Compositions with a rheological modifier to reduce dissolution variability
CN103664744B (zh) * 2013-11-30 2015-07-15 山东永泰化工有限公司 一种左布比卡因的制备方法
CA3100706A1 (en) * 2018-05-18 2019-11-21 Kura Oncology, Inc. Synthesis of tipifarnib
BR112022013784A2 (pt) 2020-01-13 2022-10-11 Durect Corp Sistemas de distribuição de fármacos de liberação prolongada com impurezas reduzidas e métodos relacionados

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE451840B (sv) * 1986-01-03 1987-11-02 Astra Laekemedel Ab Optiskt rent monohydrat av s-(-)-1-propyl-2',6'-pipekoloxylididhydroklorid, sett att framstella denna och farmaceutiska beredningar for lokalbedovning

Also Published As

Publication number Publication date
PL183204B1 (pl) 2002-06-28
DE69525950D1 (de) 2002-04-25
FI117436B (fi) 2006-10-13
AU3527995A (en) 1996-04-09
ES2173194T3 (es) 2002-10-16
PT782569E (pt) 2002-09-30
DE69525950T2 (de) 2002-09-19
US5786484A (en) 1998-07-28
NO971358L (no) 1997-03-21
EP0782569B1 (en) 2002-03-20
PL319368A1 (en) 1997-08-04
DK0782569T3 (da) 2002-07-22
CN1104416C (zh) 2003-04-02
AU695479B2 (en) 1998-08-13
NO971358D0 (no) 1997-03-21
KR100393133B1 (ko) 2003-11-17
ATE214695T1 (de) 2002-04-15
NO308074B1 (no) 2000-07-17
CA2200490C (en) 2007-01-09
WO1996009290A1 (en) 1996-03-28
CA2200490A1 (en) 1996-03-28
FI971202A (fi) 1997-03-21
JPH10505855A (ja) 1998-06-09
FI971202A0 (fi) 1997-03-21
HU216291B (hu) 1999-06-28
MX9702210A (es) 1998-05-31
HUT77055A (hu) 1998-03-02
CN1159184A (zh) 1997-09-10
EP0782569A1 (en) 1997-07-09

Similar Documents

Publication Publication Date Title
JP3898220B2 (ja) レボブピバカインおよびその類似体の製造に使用するラセミ化と不斉変換法
JP4163748B2 (ja) O,o’―ビスアロイル酒石酸類によるメチルフェニデートの光学分割
JP2001506621A (ja) エナンチオマー濃縮されたトレオ−メチルフェニデートの調製法
JP4138005B2 (ja) トレオーメチルフェニデートの分割
JP4015696B2 (ja) レボブピバカインと同類のピペリジンカルボキサニリド麻酔剤の製造に用いるラセミ化法
JPH10507464A (ja) レボブピバカインとその類似体の晶出
JP2009509958A (ja) ナフチルアルキルアミンによるα−(フェノキシ)フェニル酢酸誘導体の分割
US20030078429A1 (en) Process and diastereomeric salts useful for the optical resolution of racemic a-[4- (1,1-dimethylethy) phenyl) -4- (hydroxydipenylmethyl) -1-piperidinebutanol and derivative compounds
US6384227B2 (en) Racemisation process for use in the manufacture of levobupivacaine and related piperidinecarboxanilide anaesthetic agents
SK159899A3 (en) Process for the preparation of 4-aryl-piperidines
JP2011012032A (ja) 光学活性な3−アミノピペリジンの製造方法および製造の中間体
JP3970925B2 (ja) レボブピバカインとその類似体のl−リシンからの製造法
JPH0421662B2 (pt)
JPS5982365A (ja) 新規なラセミ分割ケト化合物およびその製法
JP4322317B2 (ja) シングルエナンチオマーナルウェジンの製造方法
JP5216762B2 (ja) (s)−1−メチル−フェニルピペラジンの立体選択的合成
JP2000504684A (ja) 第4級キラル中心のラセミ化
CA2201779C (en) The manufacture of levobupivacaine and analogues thereof from l-lysine
JP2001294582A (ja) 光学活性アミノブチロラクトンの製造法
JPH11510471A (ja) レボブピバカインおよびその前駆体のラセミ化法
KR20090023603A (ko) 네포팜과 유사체의 거울상 이성질체의 라세미화
KR20040067214A (ko) (s)-1,4-디하이드로피리딘의 제조방법

Legal Events

Date Code Title Description
A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20060411

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20060711

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20060828

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20061004

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20061121

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20061221

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20110105

Year of fee payment: 4

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20120105

Year of fee payment: 5

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20130105

Year of fee payment: 6

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20130105

Year of fee payment: 6

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

EXPY Cancellation because of completion of term